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SML2363

AST487

≥98% (HPLC)

Synonym(s):

1-(4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-(6-(methylamino)pyrimidin-4-yloxy)phenyl)urea, AST 487, AST-487, N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N′-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea, NVP-AST 487, NVP-AST-487, NVP-AST487

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About This Item

Empirical Formula (Hill Notation):
C26H30F3N7O2
CAS Number:
630124-46-8
Molecular Weight:
529.56
UNSPSC Code:
12352200
MDL number:
MFCD11983171
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC=NC(NC)=C4)C=C3)=O)C=C2)CC1

InChI

1S/C26H30F3N7O2/c1-3-35-10-12-36(13-11-35)16-18-4-5-20(14-22(18)26(27,28)29)34-25(37)33-19-6-8-21(9-7-19)38-24-15-23(30-2)31-17-32-24/h4-9,14-15,17H,3,10-13,16H2,1-2H3,(H,30,31,32)(H2,33,34,37)

InChI key

ODPGGGTTYSGTGO-UHFFFAOYSA-N

Biochem/physiol Actions

AST487 is a N,N′-diphenyl urea, which inhibits growth and calcitonin gene expression in medullary thyroid cancer cells.
AST487 is an orally available type II tyrosine kinase inhibitor (TKI) that exhibits potent antiproliferation activity against FLT3, RET, PDGFR1, but not BRAF, oncogenic fusions/mutations-driven growth (IC50 = 1.8 nM/FLT3-ITD BaF3, 5.1 nM/FLT3 D835I BaF3, 9-27 nM/TEL-PDGFR1 & PTC3-RET BaF3, <1 nM/FLT3-ITD-expressing MV4-11 &amp; MOLM-13) via binding/stablizing target kinases in the inactive “DFG-out” conformation. AST487 effectively suppresses RET- (NIH3T3-RETC634W & human medullary thyroid cancer (MTC) TT cells) and FLT3-ITD-driven (MV4-11) tumor growth in mice in vivo (20-50 mg/kg/day p.o.).
Orally active, type II tyrosine kinase inhibitor against FLT3, RET, and PDGFR1 oncogenic fusions/mutations-driven growth in vitro and in vivo.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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